Tuesday, June 5, 2012

Description of PPAHV

 PPAHV

Item name: PPAHV
CAS NO: 175796-50-6
Molecular formula: C39H44O11
Molecular weight: 688.77
Product description: PPAHV is soluble in DMSO and in ethanol and Non-pungent resiniferatoxin-type phorboid vanilloid. Agonist at rat TRPV1 (EC50 between 3 and 10?M) but virtually inactive at human TRPV1 (EC50>10?M). Induces apoptosis through a TRPV-independent mechanism. Tumor promotor.
Mutation of methionine  547 in S4 of rat TRPV1 to leucine, found in human TRPV1 (M547L), reduced the ability of PPAHV to activate TRPV1 by approximately 20 fold. The reciprocal mutation of human TRPV1 (L547M) enabled the human receptor to respond to PPAHV. These mutations did not significantly affect the agonist activity of capsaicin, resiniferatoxin (RTX) or olvanil in [Ca2+]i assays. Introducing the equivalent mutation into guinea pig TRPV1 (L549M) increased the agonist potency of PPAHV by > 10 fold in the [Ca2+]i assay and increased the amplitude of the evoked current.  The rat M547L mutation reduced the affinity of RTX binding. Determinants of capsazepine  and PPAHV function in TRPV1.
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